Assessment of catechol induction and glucuronidation in rat liver microsomes

Drug Metabolism and Disposition : the Biological Fate of Chemicals
E ElovaaraJ Taskinen

Abstract

Catechols are substances with a 1,2-dihydroxybenzene group from natural or synthetic origin. The aim of this study was to determine whether catechols (4-methylcatechol, 4-nitrocatechol, 2,3-dihydroxynaphthalene) and the antiparkinsonian drugs, entacapone and tolcapone, at doses 150 to 300 mg/kg/day, for 3 days, are able to enhance their own glucuronidation. The induction potency of catechols on rat liver UDP-glucuronosyltransferases (UGTs) was compared with that of a standard polychlorinated biphenyl (PCB) inducer, Aroclor 1254. The glucuronidation rate of these catechols was enhanced up to 15-fold in the liver microsomes of PCB-treated rats, whereas treatment with catechols had little effect. Entacapone, tolcapone, 4-methylcatechol, catechol, 2,3-dihydroxynaphthalene, and 4-nitrocatechol were glucuronidated in control microsomes at rates ranging from 0.12 for entacapone to 22.0 nmol/min/mg for 4-nitrocatechol. Using 1-naphthol, entacapone, and 1-hydroxypyrene as substrates, a 5-, 8-, and 16-fold induction was detected in the PCB rats, respectively, whereas the catechol-induced activities were 1.1- to 1.5-fold only. Entacapone was glucuronidated more efficiently by PCB microsomes than by control microsomes (Vmax/Km, 0.0125 and ...Continue Reading

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Citations

Jun 10, 2008·Journal of Pharmaceutical and Biomedical Analysis·Xuezhi BiGuifang Dou
Jun 29, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Dezhi KongLeiming Ren
Dec 6, 2011·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·J Debora van der MerweWentzel C A Gelderblom
Jul 3, 2013·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Jhodie Rubina DuncanAndrew John Lawrence
Jun 27, 2006·Telemedicine Journal and E-health : the Official Journal of the American Telemedicine Association·Justin Boyle

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